| Summary: | Abstract Many animals have evolved toxins to defend themselves from predators and hunt prey. These toxins have been honed over millions of years by the unique selective pressures on each organism leading to a vast array of potent bioactive compounds, many of which have therapeutic potential. Animal extracts have been used for medicinal purposes for thousands of years, and in the past 50 years, hundreds of animal‐derived compounds have been investigated for anticancer activity with a notable number showing significant potential. This review covers some of the most promising animal‐derived cancer therapeutic agents currently in use or under investigation. Potential therapeutic agents derived from insects, arachnids, amphibians, and marine organism are included. Four compounds are highlighted in this review: bee venom from honeybees (Apis mellifera), chlorotoxin from the Israeli deathstalker scorpion (Leiurus quinquestriatus), Huachansu from Chinese Bufo toads (Bufo bufo gargarizans and B. melanotictus), and trabectedin from the marine tunicate Ecteinascidia turbinate. For each compound, the history of their discovery, their mechanism of action, and their clinical development are discussed.
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